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Synthesis and characterization of pH-sensitive conjugate of isoniazid--methoxypoly(ethylene glycol)-b-poly(L-lysine)
A. Imramovský, L. Grusová, L. Beneš, V. Pejchal, M. Sedlák,
Language English Country England, Great Britain
Document type Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Isoniazid chemistry MeSH
- Hydrogen-Ion Concentration MeSH
- Molecular Structure MeSH
- Polyethylene Glycols chemistry MeSH
- Polylysine analogs & derivatives chemistry MeSH
- Powder Diffraction MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
The present paper deals with the preparation and characterization of a conjugate of isoniazid (INH) with the block copolymer methoxypoly(ethylene glycol)-b-poly(L-lysine) (mPEG-b-PLL). The structure of the conjugate (mPEG-b-PLL-INH) was verified by means of (1)H NMR, GPC, infrared spectroscopy, elemental analysis and powder X-ray diffraction. The conjugate contains six l-lysine units with five INH molecules, which are attached by means of pH-sensitive amidine bond. Under in vitro conditions, the conjugate is hydrolyzed and isoniazid is released (pH 4; 37 °C; t(1/2) ≈ 10 h).
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- $a The present paper deals with the preparation and characterization of a conjugate of isoniazid (INH) with the block copolymer methoxypoly(ethylene glycol)-b-poly(L-lysine) (mPEG-b-PLL). The structure of the conjugate (mPEG-b-PLL-INH) was verified by means of (1)H NMR, GPC, infrared spectroscopy, elemental analysis and powder X-ray diffraction. The conjugate contains six l-lysine units with five INH molecules, which are attached by means of pH-sensitive amidine bond. Under in vitro conditions, the conjugate is hydrolyzed and isoniazid is released (pH 4; 37 °C; t(1/2) ≈ 10 h).
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